Bouwstra J A, Honeywell-Nguyen P L
Leiden/Amsterdam Center for Drug Research, Leiden University, P O Box 9502, 2300 RA, Leiden, The Netherlands.
Adv Drug Deliv Rev. 2002 Nov 1;54 Suppl 1:S41-55. doi: 10.1016/s0169-409x(02)00114-x.
The natural function of the skin is to protect the body for unwanted influences from the environment. The main barrier of the skin is located in the outermost layer of the skin, the stratum corneum. Since the lipids regions in the stratum corneum form the only continuous structure, substances applied onto the skin always have to pass these regions. Therefore, in the first part of this paper, the barrier function has been explained, focusing on the lipid composition and organisation. The major obstacle for topical drug delivery is the low diffusion rate of drugs across the stratum corneum. Several methods have been assessed to increase the permeation rate of drugs temporarily. One of the approaches is the application of drugs in formulations containing vesicles. In order to unravel the mechanisms involved in increasing the drug transport across the skin, information on the effect of vesicles on drug permeation rate, the permeation pathway and perturbations of the skin ultrastructure is of importance. In the second part of this paper, the possible interactions between vesicles and skin are described, focusing on differences between the effects of gel-state, liquid-state, and elastic vesicles.
皮肤的自然功能是保护身体免受来自环境的有害影响。皮肤的主要屏障位于皮肤的最外层,即角质层。由于角质层中的脂质区域形成了唯一的连续结构,涂抹在皮肤上的物质总是必须穿过这些区域。因此,在本文的第一部分,已经解释了屏障功能,重点是脂质组成和结构。局部给药的主要障碍是药物穿过角质层的扩散速率低。已经评估了几种方法来暂时提高药物的渗透速率。其中一种方法是将药物应用于含有囊泡的制剂中。为了阐明增加药物经皮转运所涉及的机制,关于囊泡对药物渗透速率、渗透途径和皮肤超微结构扰动的影响的信息非常重要。在本文的第二部分,描述了囊泡与皮肤之间可能的相互作用,重点是凝胶态、液态和弹性囊泡的作用差异。